What kind of drugs does aprocitentan belong to and its main pharmacological effects?

Aprocitentan is a new type of oral antihypertensive drug that belongs to the endothelin receptor antagonist class. Its main target is the endothelin receptor, which can inhibit the vasoconstriction mediated by endothelin-1 (ET-1), thereby dilating blood vessels and lowering blood pressure. Unlike traditional antihypertensive drugs, aprecitentan not only regulates vascular tension, but also has a certain protective effect on the cardiovascular system, providing a new treatment option for patients with refractory hypertension.

Pharmacologically, aprecitentan achieves vasodilation and anti-remodeling effects by simultaneously blocking ETA and ETB receptors. ETAReceptor blockade can reduce peripheral vascular resistance and improve cardiac load; ETBReceptor blockade can reduce water and sodium retention and vasoconstriction signal conduction, thereby helping to maintain blood pressure stability. Preclinical and early-stage studies have shown that the drug can effectively improve blood pressure control in long-term use, while also having a protective effect on cardiac structure and vascular function, reducing the risk of complications caused by hypertension.

The pharmacokinetic properties of aprecitentan also show that it is well absorbed orally, has high bioavailability, and its plasma concentration can be maintained in the body for a long time, thus supporting a once or twice daily oral regimen. It is metabolized by the liver and excreted in bile and urine. Patients with mild to moderate renal impairment do not need to adjust the dosage. However, patients with severe renal or hepatic insufficiency need to use it with caution to avoid accumulation of the drug in the body and lead to adverse reactions.

Overall, aprecitentan, as an endothelin receptor antagonist, has unique advantages in antihypertensive treatment. It can not only significantly reduce blood pressure, but also improve vasodilation function, and is suitable for patients with refractory hypertension or in whom other conventional antihypertensive drugs are ineffective. With the accumulation of more clinical studies and data, aprecitentan is expected to become a new treatment option in the cardiovascular field, while providing patients with a safer and more efficient blood pressure management solution.

Reference materials:https://go.drugbank.com/drugs/DB15059